BR9812048A - Compound, use of it, pharmaceutical composition, and, processes of treating a disease mediated by a kinase, of treating rejection in organ transplantation, and of treating chemotherapy-induced alopecia - Google Patents
Compound, use of it, pharmaceutical composition, and, processes of treating a disease mediated by a kinase, of treating rejection in organ transplantation, and of treating chemotherapy-induced alopeciaInfo
- Publication number
- BR9812048A BR9812048A BR9812048-4A BR9812048A BR9812048A BR 9812048 A BR9812048 A BR 9812048A BR 9812048 A BR9812048 A BR 9812048A BR 9812048 A BR9812048 A BR 9812048A
- Authority
- BR
- Brazil
- Prior art keywords
- aliphatic
- treating
- aminosulfonyl
- sulfonyl
- chemotherapy
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 201000010099 disease Diseases 0.000 title abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 3
- 230000001404 mediated effect Effects 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- 102000001253 Protein Kinase Human genes 0.000 title abstract 2
- 208000022605 chemotherapy-induced alopecia Diseases 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 210000000056 organ Anatomy 0.000 title abstract 2
- 108060006633 protein kinase Proteins 0.000 title abstract 2
- 238000002054 transplantation Methods 0.000 title abstract 2
- 125000001931 aliphatic group Chemical group 0.000 abstract 8
- -1 aminosulfonylamino Chemical group 0.000 abstract 3
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 201000004384 Alopecia Diseases 0.000 abstract 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 abstract 1
- 102000015792 Cyclin-Dependent Kinase 2 Human genes 0.000 abstract 1
- 108010024986 Cyclin-Dependent Kinase 2 Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 231100000360 alopecia Toxicity 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 238000002512 chemotherapy Methods 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 238000001959 radiotherapy Methods 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/32—Oxygen atoms
- C07D209/34—Oxygen atoms in position 2
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/40—Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
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- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Biomedical Technology (AREA)
- Ophthalmology & Optometry (AREA)
- Rheumatology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Toxicology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Cosmetics (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
"COMPOSTO, USO DO MESMO, COMPOSIçãO FARMACêUTICA, E, PROCESSOS DE TRATAR UMA DOENçA MEDIADA POR UMA CINASE, DE TRATAR A REJEIçãO NO TRANSPLANTE DE óRGãO, E DE TRATAR A ALOPECIA INDUZIDA PELA QUIMIOTERAPIA" Os compostos da fórmula (1): em que X é N, CH, CCF~ 3~ ou C(alifático C~ 1-12~); R^ 4^ é ácido sulfónico, alifático C~ 1-12~ sulfonila, sulfonila C~ 1-12~ alifático, alifático C~ 1-12~ sulfonila C~ 1-6~alifático, alifático C~ 1-6~ amino, R^ 7^-sulfonila, R^ 7^-sulfonila alifático C~ 1-12~, R^ 7^-aminossulfonila, R^ 7^-aminossulfonila alifático C~ 1-12~, R^ 7^-sulfonilamino, R^ 7^-sulfonilamino alifático C~ 1-12~, aminossulfonilamino, amino di-alifático C~ 1-12~, aminocarbonila di-alifático C~ 1-12~, aminossulfonila di-alifático C~ 1-12~, amino di-alifático C~ 1-12~, aminocarbonila di-alifático C~ 1-12~, alifático C~ 1-12~ aminossulfonila di-alifático C~ 1-12~, (R^ 8^)~ 1-3~-arilamino, (R^ 8^)~ 1-3~-arilsulfonila, (R^ 8^)~ 1-3~-aril-aminisulfonila, (R^ 8^)~ 1-3~-aril-sulfonilamino, Het-amino, Het-sulfonila, Het-aminossulfonila, aminoiminoamino ou aminoiminoaminossulfonila, R^ 5^ é hidrogênio e ainda em que R^ 4^ e R^ 5^ estão opcionalmente unidos para formar um anel fundido, formulações farmacêuticas que os compreendem, seus usos em terapia, especialmente no tratamento de doenças mediadas pela atividade CDK2, tais como alopecia induzida pela quimioterapia ou radioterapia contra o câncer."COMPOUND, USE OF THE SAME, PHARMACEUTICAL COMPOSITION, AND, PROCESSES OF TREATING A DISEASE MEDIATED BY A KINASE, OF TREATING REJECTION IN ORGAN TRANSPLANTATION, AND OF TREATING CHEMOTHERAPY-INDUCED ALOPECIA" in the compounds of the formula (1) X is N, CH, CCF ~ 3 ~ or C (aliphatic C ~ 1-12 ~); R ^ 4 ^ is sulfonic acid, aliphatic C ~ 1-12 ~ sulfonyl, sulfonyl C ~ 1-12 ~ aliphatic, aliphatic C ~ 1-12 ~ sulfonyl C ~ 1-6 ~ aliphatic, aliphatic C ~ 1-6 ~ amino , R ^ 7 ^ -sulfonyl, R ^ 7 ^ -aliphatic C ~ 1-12 ~, R ^ 7 ^ -aminosulfonyl, R ^ 7 ^ -aminosulfonyl C ~ 1-12 ~, R ^ 7 ^ -sulfonylamino, R ^ 7 ^ -Aliphatic C ~ 1-12 ~ aliphatic, aminosulfonylamino, C ~ 1-12 ~ di-aliphatic amino, C ~ 1-12 ~ di-aliphatic aminocarbonyl, C ~ 1-12 ~ di-aliphatic aminosulfonyl, amino di-aliphatic C ~ 1-12 ~, aminocarbonyl di-aliphatic C ~ 1-12 ~, aliphatic C ~ 1-12 ~ aminosulfonyl di-aliphatic C ~ 1-12 ~, (R ^ 8 ^) ~ 1-3 ~ -arylamino, (R ^ 8 ^) ~ 1-3 ~ -arylsulfonyl, (R ^ 8 ^) ~ 1-3 ~ -aryl-aminisulfonyl, (R ^ 8 ^) ~ 1-3 ~ -aryl-sulfonylamino, Het -amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino or aminoiminoaminosulfonyl, R ^ 5 ^ is hydrogen and in which R ^ 4 ^ and R ^ 5 ^ are optionally joined to form a fused ring, pharmaceutical formulations that comprise them, their uses in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by chemotherapy or radiation therapy against cancer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9718913.8A GB9718913D0 (en) | 1997-09-05 | 1997-09-05 | Substituted oxindole derivatives |
| PCT/EP1998/005559 WO1999015500A1 (en) | 1997-09-05 | 1998-09-03 | Substituted oxindole derivatives as protein tyrosine kinase and as protein serine/threonine kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR9812048A true BR9812048A (en) | 2000-09-26 |
Family
ID=10818643
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR9812048-4A BR9812048A (en) | 1997-09-05 | 1998-09-03 | Compound, use of it, pharmaceutical composition, and, processes of treating a disease mediated by a kinase, of treating rejection in organ transplantation, and of treating chemotherapy-induced alopecia |
Country Status (23)
| Country | Link |
|---|---|
| US (4) | US6387919B1 (en) |
| EP (1) | EP1009738B1 (en) |
| JP (1) | JP2001517652A (en) |
| KR (1) | KR20010023695A (en) |
| CN (1) | CN1278794A (en) |
| AR (1) | AR015432A1 (en) |
| AT (1) | ATE267170T1 (en) |
| AU (1) | AU747506B2 (en) |
| BR (1) | BR9812048A (en) |
| CA (1) | CA2302572A1 (en) |
| CO (1) | CO4960633A1 (en) |
| DE (1) | DE69824014T2 (en) |
| EE (1) | EE200000117A (en) |
| ES (1) | ES2221211T3 (en) |
| GB (1) | GB9718913D0 (en) |
| HU (1) | HUP0004490A3 (en) |
| MA (1) | MA26542A1 (en) |
| PE (1) | PE107699A1 (en) |
| PL (1) | PL338991A1 (en) |
| TR (1) | TR200001174T2 (en) |
| TW (1) | TW520358B (en) |
| WO (1) | WO1999015500A1 (en) |
| ZA (1) | ZA988078B (en) |
Families Citing this family (266)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6407132B1 (en) * | 1997-07-25 | 2002-06-18 | James Black Foundation Limited | Substituted imidazole derivatives and their use as histamine H3 receptor ligands |
| GB9718913D0 (en) * | 1997-09-05 | 1997-11-12 | Glaxo Group Ltd | Substituted oxindole derivatives |
| DE19816624A1 (en) * | 1998-04-15 | 1999-10-21 | Boehringer Ingelheim Pharma | Novel substituted indolinones, their preparation and their use as pharmaceuticals |
| DE19824922A1 (en) * | 1998-06-04 | 1999-12-09 | Boehringer Ingelheim Pharma | Novel substituted indolinones, their preparation and their use as pharmaceuticals |
| US6319918B1 (en) | 1998-06-04 | 2001-11-20 | Boehringer Ingelheim Pharma Kg | Substituted indolinones with kinase inhibitory activity |
| CN1158283C (en) * | 1998-12-17 | 2004-07-21 | 霍夫曼-拉罗奇有限公司 | 4-and 5-pyrazinyl oxindoles as protein kinase inhibitors |
| US6153634A (en) | 1998-12-17 | 2000-11-28 | Hoffmann-La Roche Inc. | 4,5-azolo-oxindoles |
| DE69906152T2 (en) | 1998-12-17 | 2004-02-12 | F. Hoffmann-La Roche Ag | 4-ALKENYL (AND ALKINYL) OXOINDOLE AS INHIBITORS CYCLINE-DEPENDENT KINASES, ESPECIALLY CDK2 |
| KR100685192B1 (en) * | 1998-12-17 | 2007-02-22 | 에프. 호프만-라 로슈 아게 | 4,5-azolo-oxindole |
| BR9916223A (en) | 1998-12-17 | 2001-09-04 | Hoffmann La Roche | 4-aryloxindols as inhibitors of jnk protein kinases |
| DE60045474D1 (en) | 1999-01-13 | 2011-02-17 | Univ New York State Res Found | NEW METHOD FOR CREATING PROTEIN KINASE INHIBITORS |
| GB9904932D0 (en) * | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Composition and method for preventing/reducing the severity of side effects of chemotherapy and/or radiation therapy |
| GB9904933D0 (en) | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Compounds |
| GB9904930D0 (en) * | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Thiazoloindolinone compounds |
| US6492398B1 (en) * | 1999-03-04 | 2002-12-10 | Smithkline Beechman Corporation | Thiazoloindolinone compounds |
| US6624171B1 (en) | 1999-03-04 | 2003-09-23 | Smithkline Beecham Corporation | Substituted aza-oxindole derivatives |
| US6423699B1 (en) | 1999-05-04 | 2002-07-23 | American Home Products Corporation | Combination therapies using benzimidazolones |
| US6498154B1 (en) | 1999-05-04 | 2002-12-24 | Wyeth | Cyclic regimens using quinazolinone and benzoxazine derivatives |
| US6306851B1 (en) | 1999-05-04 | 2001-10-23 | American Home Products Corporation | Cyclocarbamate and cyclic amide derivatives |
| US6358947B1 (en) | 1999-05-04 | 2002-03-19 | American Home Products Corporation | Tetracyclic progesterone receptor modulator compounds and methods |
| US6417214B1 (en) | 1999-05-04 | 2002-07-09 | Wyeth | 3,3-substituted indoline derivatives |
| US6391907B1 (en) | 1999-05-04 | 2002-05-21 | American Home Products Corporation | Indoline derivatives |
| US6509334B1 (en) | 1999-05-04 | 2003-01-21 | American Home Products Corporation | Cyclocarbamate derivatives as progesterone receptor modulators |
| US6380235B1 (en) | 1999-05-04 | 2002-04-30 | American Home Products Corporation | Benzimidazolones and analogues |
| US6355648B1 (en) | 1999-05-04 | 2002-03-12 | American Home Products Corporation | Thio-oxindole derivatives |
| US6329416B1 (en) | 1999-05-04 | 2001-12-11 | American Home Products Corporation | Combination regimens using 3,3-substituted indoline derivatives |
| US6339098B1 (en) | 1999-05-04 | 2002-01-15 | American Home Products Corporation | 2,1-benzisothiazoline 2,2-dioxides |
| US6358948B1 (en) | 1999-05-04 | 2002-03-19 | American Home Products Corporation | Quinazolinone and benzoxazine derivatives as progesterone receptor modulators |
| US6369056B1 (en) | 1999-05-04 | 2002-04-09 | American Home Products Corporation | Cyclic urea and cyclic amide derivatives |
| US6380178B1 (en) | 1999-05-04 | 2002-04-30 | American Home Products Corporation | Cyclic regimens using cyclocarbamate and cyclic amide derivatives |
| US6319912B1 (en) | 1999-05-04 | 2001-11-20 | American Home Products Corporation | Cyclic regimens using 2,1-benzisothiazoline 2,2-dioxides |
| US6462032B1 (en) | 1999-05-04 | 2002-10-08 | Wyeth | Cyclic regimens utilizing indoline derivatives |
| US6399593B1 (en) | 1999-05-04 | 2002-06-04 | Wyeth | Cyclic regimens using cyclic urea and cyclic amide derivatives |
| US6407101B1 (en) | 1999-05-04 | 2002-06-18 | American Home Products Corporation | Cyanopyrroles |
| US6444668B1 (en) | 1999-05-04 | 2002-09-03 | Wyeth | Combination regimens using progesterone receptor modulators |
| GB9911053D0 (en) | 1999-05-12 | 1999-07-14 | Pharmacia & Upjohn Spa | 4,5,6,7-tetrahydroindazole derivatives process for their preparation and their use as antitumour agents |
| DE19924401A1 (en) * | 1999-05-27 | 2000-11-30 | Boehringer Ingelheim Pharma | Novel substituted indolinones, their preparation and their use as pharmaceuticals |
| DE50012136D1 (en) * | 1999-08-27 | 2006-04-13 | Boehringer Ingelheim Pharma | Substituierte indolinone als tyrosinkinase inhibitoren |
| AU771460B2 (en) * | 1999-09-24 | 2004-03-25 | Smithkline Beecham Corporation | Thrombopoietin mimetics |
| DE19949209A1 (en) * | 1999-10-13 | 2001-04-19 | Boehringer Ingelheim Pharma | 5-substituted indolinones, their preparation and their use as pharmaceuticals |
| US6762180B1 (en) | 1999-10-13 | 2004-07-13 | Boehringer Ingelheim Pharma Kg | Substituted indolines which inhibit receptor tyrosine kinases |
| UA75054C2 (en) * | 1999-10-13 | 2006-03-15 | Бьорінгер Інгельхайм Фарма Гмбх & Ко. Кг | Substituted in position 6 indolinones, producing and use thereof as medicament |
| US6313310B1 (en) | 1999-12-15 | 2001-11-06 | Hoffmann-La Roche Inc. | 4-and 5-alkynyloxindoles and 4-and 5-alkenyloxindoles |
| YU54202A (en) | 2000-01-18 | 2006-01-16 | Agouron Pharmaceuticals Inc. | Indazole compounds,pharmaceutical compositions,and methods for mediating or inhibiting cell proliferation |
| HN2001000008A (en) | 2000-01-21 | 2003-12-11 | Inc Agouron Pharmaceuticals | AMIDA COMPOSITE AND PHARMACEUTICAL COMPOSITIONS TO INHIBIT PROTEINKINASES, AND THE INSTRUCTIONS FOR USE |
| WO2001056557A2 (en) * | 2000-02-05 | 2001-08-09 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of erk |
| US6620818B1 (en) * | 2000-03-01 | 2003-09-16 | Smithkline Beecham Corporation | Method for reducing the severity of side effects of chemotherapy and/or radiation therapy |
| CA2398446A1 (en) | 2000-04-18 | 2001-10-25 | Agouron Pharmaceuticals, Inc. | Pyrazoles for inhibiting protein kinases |
| UA73119C2 (en) | 2000-04-19 | 2005-06-15 | American Home Products Corpoir | Derivatives of cyclic thiocarbamates, pharmaceutical composition including noted derivatives of cyclic thiocarbamates and active ingredients of medicines as modulators of progesterone receptors |
| US6534531B2 (en) * | 2000-04-27 | 2003-03-18 | Bristol-Myers Squibb Company | Methods for preventing and treating alopecia induced by chemotherapy or radiotherapy |
| AU2001252562A1 (en) * | 2000-04-28 | 2001-11-12 | Toshiharu Suzuki | Medicinal compositions for suppressing beta-amyloid production |
| CY2010012I2 (en) | 2000-05-25 | 2020-05-29 | Novartis Ag | THROMBOPOIETIN MIMETICS |
| GB0016454D0 (en) | 2000-07-04 | 2000-08-23 | Hoffmann La Roche | Thienopyrrolidinones |
| CA2411928A1 (en) | 2000-08-09 | 2002-02-14 | Agouron Pharmaceuticals, Inc. | Pyrazole-thiazole compounds, pharmaceutical compositions containing them, and methods of their use for inhibiting cyclindependent kinases |
| MXPA03001452A (en) | 2000-08-18 | 2004-05-04 | Agouron Pharma | Heterocyclic-hydroxyimino-fluorenes and their use for inhibiting protein kinases. |
| US6964977B2 (en) | 2000-09-01 | 2005-11-15 | Smithkline Beecham Corporation | Oxindole derivatives |
| AU2001288374A1 (en) | 2000-09-01 | 2002-03-22 | Glaxo Group Limited | Substituted oxindole derivatives as tyrosine kinase inhibitors |
| JP2004508372A (en) | 2000-09-01 | 2004-03-18 | グラクソ グループ リミテッド | Oxindole derivatives |
| EP1201765A3 (en) * | 2000-10-16 | 2003-08-27 | Axxima Pharmaceuticals Aktiengesellschaft | Cellular kinases involved in cytomegalovirus infection and their inhibition |
| DE10054019A1 (en) * | 2000-11-01 | 2002-05-23 | Boehringer Ingelheim Pharma | New substituted indolinones, their production and their use as medicines |
| US6638965B2 (en) | 2000-11-01 | 2003-10-28 | Boehringer Ingelheim Pharma Kg | Substituted indolinones, preparation thereof and their use as pharmaceutical compositions |
| DE10117204A1 (en) * | 2001-04-06 | 2002-10-10 | Boehringer Ingelheim Pharma | Indolinones substituted in the 6-position, their preparation and their use as medicaments |
| SE0101230L (en) * | 2001-04-06 | 2002-10-07 | Innoventus Project Ab | New use of a tyrosine kinase inhibitor |
| CA2448076A1 (en) * | 2001-05-24 | 2002-11-28 | Masahiko Hayakawa | 3-quinoline-2-(1h)-ylideneindolin-2-one derivatives |
| US7727731B2 (en) | 2001-06-29 | 2010-06-01 | Ab Science | Potent, selective and non toxic c-kit inhibitors |
| EP1401415B1 (en) | 2001-06-29 | 2006-06-21 | AB Science | Use of n-phenyl-2-pyrimidine-amine derivatives for treating inflammatory diseases |
| US7678805B2 (en) | 2001-06-29 | 2010-03-16 | Ab Science | Use of tyrosine kinase inhibitors for treating inflammatory bowel diseases (IBD) |
| DE60225590T2 (en) * | 2001-09-20 | 2008-09-25 | Ab Science | C-KITHEMMER FOR THE TREATMENT OF BACTERIAL INFECTIONS |
| ATE401078T1 (en) * | 2001-09-20 | 2008-08-15 | Ab Science | THE USE OF C-KIT INHIBITORS TO PROMOTE HAIR GROWTH |
| WO2003027109A1 (en) * | 2001-09-27 | 2003-04-03 | Allergan, Inc. | 3-(heteroarylamino)methylene-1, 3-dihydro-2h-indol-2-ones as kinase inhibitors |
| US20030225152A1 (en) * | 2001-09-27 | 2003-12-04 | Andrews Steven W. | 3-(Arylamino)methylene-1, 3-dihydro-2h-indol-2-ones as kinase inhibitors |
| WO2003033491A1 (en) * | 2001-10-16 | 2003-04-24 | Nippon Kayaku Kabushiki Kaisha | Medicinal composition for prevention or alleviation of side effect of antitumor and medicinal antitumor composition |
| US7005445B2 (en) | 2001-10-22 | 2006-02-28 | The Research Foundation Of State University Of New York | Protein kinase and phosphatase inhibitors and methods for designing them |
| JP4623962B2 (en) * | 2001-10-22 | 2011-02-02 | ザ・リサーチ・ファウンデーション・オブ・ステイト・ユニバーシティ・オブ・ニューヨーク | Protein kinases and phosphatase inhibitors, methods of designing them, and methods of using them |
| US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
| US6797825B2 (en) | 2001-12-13 | 2004-09-28 | Abbott Laboratories | Protein kinase inhibitors |
| US20050070591A1 (en) * | 2001-12-18 | 2005-03-31 | Fumihiko Kanai | Indole derivative |
| WO2003059884A1 (en) | 2001-12-21 | 2003-07-24 | X-Ceptor Therapeutics, Inc. | Modulators of lxr |
| US7482366B2 (en) * | 2001-12-21 | 2009-01-27 | X-Ceptor Therapeutics, Inc. | Modulators of LXR |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| FR2836914B1 (en) | 2002-03-11 | 2008-03-14 | Aventis Pharma Sa | SUBSTITUTED INDAZOLES, COMPOSITIONS CONTAINING SAME, METHOD OF MANUFACTURE AND USE |
| KR20040104566A (en) * | 2002-04-30 | 2004-12-10 | 알콘, 인코퍼레이티드 | Agents which regulate, inhibit, or modulate the activity and/or expression of connective tissue growth factor(CTGF) as a unique means to both lower intraocular pressure and treat glaucomatous retinopathies/optic neuropathies |
| AR040083A1 (en) | 2002-05-22 | 2005-03-16 | Smithkline Beecham Corp | BIS- (MONOETHANOLAMINE) ACID COMPOUND 3 '- [(2Z) - [1- (3,4-DIMETHYLPHENYL) -1,5-DIHIDRO-3-METHYL-5-OXO-4H-PIRAZOL-4-ILIDEN] HYDRAZINE ] -2'-HYDROXI- [1,1'-BIFENIL] -3-CARBOXILICO, PROCEDURE TO PREPARE IT, PHARMACEUTICAL COMPOSITION THAT INCLUDES IT, PROCEDURE TO PREPARE SUCH FARMAC COMPOSITION |
| US7169936B2 (en) | 2002-07-23 | 2007-01-30 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Indolinone derivatives substituted in the 6-position, their preparation and their use as medicaments |
| US7514468B2 (en) | 2002-07-23 | 2009-04-07 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Indolinone derivatives substituted in the 6 position, the preparation thereof and their use as pharmaceutical compositions |
| DE10233500A1 (en) * | 2002-07-24 | 2004-02-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 3-Z- [1- (4- (N - ((4-methyl-piperazin-1-yl) -methylcarbonyl) -N-methyl-amino) -anilino) -1-phenyl-methylene] -6-methoxycarbonyl- 2-indolinone monoethanesulfonate and its use as a medicament |
| TW200410937A (en) * | 2002-08-07 | 2004-07-01 | Synaptic Pharma Corp | 3-imino-2-indolones for the treatment of depression and/or anxiety |
| US20040082615A1 (en) * | 2002-08-07 | 2004-04-29 | Michael Konkel | 3-Imino-2-indolones for the treatement of depression and/or anxiety |
| GB0225873D0 (en) * | 2002-11-06 | 2002-12-11 | Cyclacel Ltd | Combination |
| WO2004048366A1 (en) * | 2002-11-22 | 2004-06-10 | Yamanouchi Pharmaceutical Co., Ltd. | 2-oxoindoline derivatives |
| AU2003290304A1 (en) | 2002-12-23 | 2004-07-14 | Astex Technology Limited | Synthesis and screening of ligands using x-ray crystallography |
| AU2004265288A1 (en) | 2003-07-30 | 2005-02-24 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases |
| TW200526638A (en) | 2003-10-22 | 2005-08-16 | Smithkline Beecham Corp | 2-(3,4-dimethylphenyl)-4-{[2-hydroxy-3'-(1H-tetrazol-5-yl)biphenyl-3-yl]-hydrazono}-5-methyl-2,4-dihydropyrazol-3-one choline |
| GB0328180D0 (en) * | 2003-12-04 | 2004-01-07 | Cyclacel Ltd | Combination |
| DE102004012069A1 (en) * | 2004-03-12 | 2005-09-29 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | New aryl-containing 5-acylindolinones, their preparation and their use as pharmaceuticals |
| WO2005118551A2 (en) * | 2004-05-28 | 2005-12-15 | Ligand Pharmaceuticals Inc. | Thrombopoietin activity modulating compounds and methods |
| NZ554662A (en) * | 2004-10-25 | 2008-11-28 | Ligand Pharm Inc | Thrombopoietin activity modulating compounds and methods |
| GT200500321A (en) * | 2004-11-09 | 2006-09-04 | COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF PROTEIN KINASE. | |
| CA2588517A1 (en) | 2004-12-01 | 2006-06-08 | Devgen N.V. | 5-carboxamido substituted thiazole derivatives that interact with ion channels, in particular with ion channels from the kv family |
| JP4326575B2 (en) | 2004-12-17 | 2009-09-09 | デブゲン・エヌ・ブイ | Nematicidal composition |
| PE20060777A1 (en) * | 2004-12-24 | 2006-10-06 | Boehringer Ingelheim Int | INDOLINONE DERIVATIVES FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES |
| WO2006101937A1 (en) * | 2005-03-18 | 2006-09-28 | Janssen Pharmaceutica N.V. | Acylhydrazones as kinase modulators |
| WO2006119660A1 (en) * | 2005-05-11 | 2006-11-16 | Givaudan Sa | Encapsulation method |
| US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| NZ563454A (en) | 2005-06-08 | 2011-03-31 | Rigel Pharmaceuticals Inc | 2,4-diaminopyrimidine derivatives for inhibition of the JAK pathway |
| EP1902025A1 (en) * | 2005-07-13 | 2008-03-26 | Allergan, Inc. | Kinase inhibitors |
| US7749530B2 (en) | 2005-07-13 | 2010-07-06 | Allergan, Inc. | Kinase inhibitors |
| WO2007008985A2 (en) * | 2005-07-13 | 2007-01-18 | Allergan, Inc. | Kinase inhibitors |
| GB0523041D0 (en) * | 2005-11-11 | 2005-12-21 | Cyclacel Ltd | Combination |
| CA2642229C (en) | 2006-02-24 | 2015-05-12 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| US8987474B2 (en) * | 2006-04-07 | 2015-03-24 | University Of South Florida | Inhibition of Shp2/PTPN11 protein tyrosine phosphatase by NSC-87877, NSC-117199 and their analogs |
| US7838542B2 (en) | 2006-06-29 | 2010-11-23 | Kinex Pharmaceuticals, Llc | Bicyclic compositions and methods for modulating a kinase cascade |
| US8217177B2 (en) * | 2006-07-14 | 2012-07-10 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| US8036664B2 (en) * | 2006-09-22 | 2011-10-11 | Kineto Wireless, Inc. | Method and apparatus for determining rove-out |
| WO2008045627A2 (en) * | 2006-10-06 | 2008-04-17 | Irm Llc | Protein kinase inhibitors and methods for using thereof |
| GB0625283D0 (en) * | 2006-12-19 | 2007-01-24 | Cyclacel Ltd | Combination |
| HRP20110709T1 (en) * | 2007-02-13 | 2011-11-30 | Ab Science | PROCESS OF SYNTHESIS OF 2-AMINOTHYAZOL COMPOUNDS AS KINASE INHIBITOR |
| US20100143440A1 (en) * | 2007-04-30 | 2010-06-10 | The Uab Research Foundation | Ul97 inhibitors for treatment of proliferative disorders |
| ECSP077628A (en) | 2007-05-03 | 2008-12-30 | Smithkline Beechman Corp | NEW PHARMACEUTICAL COMPOSITION |
| US7863315B2 (en) * | 2008-01-15 | 2011-01-04 | Shenzhen Chipscreen Biosciences, Ltd. | 2-indolinone derivatives as selective histone deacetylase inhibitors |
| LT2265607T (en) | 2008-02-15 | 2017-03-27 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases |
| US20110092452A1 (en) * | 2008-03-05 | 2011-04-21 | The Regents Of The University Of Michigan | Compositions and methods for diagnosing and treating pancreatic cancer |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| AU2009244897B2 (en) | 2008-04-16 | 2014-11-13 | Alexion Pharmaceuticals, Inc. | 2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors |
| EP2116236A1 (en) | 2008-04-21 | 2009-11-11 | Université de Mons-Hainaut | Bisbenzamidine derivatives for use as antioxidant |
| EP2271631B1 (en) | 2008-04-22 | 2018-07-04 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| WO2009135000A2 (en) * | 2008-04-30 | 2009-11-05 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Inhibition of shp2/ptpn11 protein tyrosine phosphatase by nsc-117199 and analogs |
| WO2009139834A1 (en) * | 2008-05-13 | 2009-11-19 | Poniard Pharmaceuticals, Inc. | Bioactive compounds for treatment of cancer and neurodegenerative diseases |
| PL2307002T3 (en) | 2008-06-09 | 2013-05-31 | Cyclacel Ltd | Combinations of sapacitabine or cndac with dna methyltransferase inhibitors such as decitabine and procaine |
| US20110224221A1 (en) * | 2008-10-01 | 2011-09-15 | Sharpless Norman E | Hematopoietic protection against ionizing radiation using selective cyclin-dependent kinase 4/6 inhibitors |
| EP2341911A4 (en) * | 2008-10-01 | 2012-10-24 | Univ North Carolina | HEMATOPOIETIC PROTECTION AGAINST CHEMOTHERAPEUTIC COMPOUNDS USING SELF-ACTIVE CYCLINE-DEPENDENT KINASE-4/6 INHIBITORS |
| WO2010121212A2 (en) | 2009-04-17 | 2010-10-21 | H. Lee Moffit Cancer Center And Research Institute, Inc. | Indoline scaffold shp-2 inhibitors and method of treating cancer |
| AU2010248886A1 (en) * | 2009-05-13 | 2011-12-01 | The University Of North Carolina At Chapel Hill | Cyclin dependent kinase inhibitors and methods of use |
| JP2012528184A (en) | 2009-05-29 | 2012-11-12 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Methods of administration of thrombopoietin agonist compounds |
| CN106420756A (en) * | 2009-07-28 | 2017-02-22 | 里格尔药品股份有限公司 | Compositions and methods for inhibition of the JAK pathway |
| BR112012007160A2 (en) | 2009-09-30 | 2018-03-13 | Harvard College | methods for modulating autophagy by modulating autophagy inhibitor gene products |
| US8652534B2 (en) | 2009-10-14 | 2014-02-18 | Berry Pharmaceuticals, LLC | Compositions and methods for treatment of mammalian skin |
| SI2493895T1 (en) * | 2009-10-29 | 2017-10-30 | Vectura Limited | N-containing heteroaryl derivatives as jak3 kinase inhibitors |
| US20120328568A1 (en) | 2010-02-12 | 2012-12-27 | Emory University | Compositions and uses of lectins |
| MX2012010174A (en) | 2010-03-02 | 2012-11-30 | Amakem Nv | Heterocyclic amides as rock inhibitors. |
| WO2011161256A1 (en) | 2010-06-25 | 2011-12-29 | Facultes Universitaires Notre Dame De La Paix | Beta carboline derivatives useful in the treatment of proliferative disorders |
| US8785648B1 (en) | 2010-08-10 | 2014-07-22 | The Regents Of The University Of California | PKC-epsilon inhibitors |
| US9511071B2 (en) | 2010-08-18 | 2016-12-06 | Emory University | Compounds and compositions for ossification and methods related thereto |
| WO2012022780A1 (en) | 2010-08-19 | 2012-02-23 | Université Libre de Bruxelles | 18-beta-glycyrrhetinic acid derivatives with anti-tumor activity |
| US8691830B2 (en) | 2010-10-25 | 2014-04-08 | G1 Therapeutics, Inc. | CDK inhibitors |
| HUE030714T2 (en) | 2010-10-25 | 2017-05-29 | G1 Therapeutics Inc | CDK inhibitors |
| EP2632466A4 (en) | 2010-10-29 | 2014-03-19 | Univ Emory | QUINAZOLINE DERIVATIVES, COMPOSITIONS AND USES THEREOF |
| WO2012061428A2 (en) | 2010-11-01 | 2012-05-10 | Portola Pharmaceuticals, Inc. | Nicotinamides as jak kinase modulators |
| GB201019043D0 (en) | 2010-11-10 | 2010-12-22 | Protea Biopharma N V | Use of 2',5'-oligoadenylate derivative compounds |
| AU2011329763A1 (en) | 2010-11-17 | 2013-05-09 | Brigham And Women's Hospital | Protection of renal tissues from ischemia through inhibition of the proliferative kinases CDK4 and CDK6 |
| WO2012075362A2 (en) | 2010-12-03 | 2012-06-07 | Emory University | Chemokine cxcr4 receptor modulators and used related thereto |
| US8691777B2 (en) | 2011-01-27 | 2014-04-08 | Emory University | Combination therapy |
| WO2012116135A2 (en) | 2011-02-24 | 2012-08-30 | Emory University | Noggin blocking compositions for ossification and methods related thereto |
| EP2678052B1 (en) | 2011-02-24 | 2018-09-26 | Emory University | Jab1 blocking compositions for ossification and methods related thereto |
| WO2012135296A2 (en) | 2011-03-31 | 2012-10-04 | Emory University | Imidazolyl amide compounds and uses related thereto |
| JP6093755B2 (en) | 2011-04-14 | 2017-03-08 | サイクラセル リミテッド | Administration regimen of a combination of sapacitabine and decitabine to treat acute myeloid leukemia |
| EP2699539B1 (en) | 2011-04-21 | 2019-03-06 | Emory University | Cyclopropyl derivatives and methods of use |
| GB201107223D0 (en) | 2011-04-29 | 2011-06-15 | Amakem Nv | Novel rock inhibitors |
| AU2012252433A1 (en) | 2011-05-09 | 2013-11-07 | Universiteit Antwerpen | Activity-based probes for the urokinase plasminogen activator |
| GB201108225D0 (en) | 2011-05-17 | 2011-06-29 | Amakem Nv | Novel KBC inhibitors |
| CA2839956A1 (en) | 2011-06-20 | 2012-12-27 | Emory University | Prostaglandin receptor ep2 antagonists, derivatives, compositions, and uses related thereto |
| GB201113689D0 (en) | 2011-08-09 | 2011-09-21 | Amakem Nv | Novel PDE4 inhibitors |
| US9040567B2 (en) | 2011-08-19 | 2015-05-26 | Emory University | BAX agonist, compositions, and methods related thereto |
| GB201114854D0 (en) | 2011-08-29 | 2011-10-12 | Amakem Nv | Novel rock inhibitors |
| JP2014525425A (en) | 2011-08-31 | 2014-09-29 | アマケン エンヴェー | Novel ROCK kinase inhibitor |
| EA025881B1 (en) | 2011-09-30 | 2017-02-28 | Онкодизайн С.А. | Macrocyclic flt3 kinase inhibitors |
| HUE029728T2 (en) | 2011-09-30 | 2017-03-28 | Ipsen Pharma Sas | Macrocyclic lrrk2 kinase inhibitors |
| GB201119358D0 (en) | 2011-11-10 | 2011-12-21 | Lewi Paulus J | Disubstituted triazine dimers for treatment and/or prevention of infectious diseases |
| DE102011119127A1 (en) * | 2011-11-22 | 2013-05-23 | Merck Patent Gmbh | 3-Cyanaryl-1H-pyrrolo [2,3-b] pyridine derivatives |
| JP6039683B2 (en) | 2011-11-23 | 2016-12-07 | ポートラ ファーマシューティカルズ, インコーポレイテッド | Pyrazine kinase inhibitor |
| ES2958619T3 (en) | 2012-01-30 | 2024-02-12 | Univ Gent | Anti-invasive compounds |
| GB201204756D0 (en) | 2012-03-19 | 2012-05-02 | Lewi Paulus J | Triazines with suitable spacers for treatment and/or prevention of HIV infections |
| CA2868966C (en) | 2012-03-29 | 2021-01-26 | Francis Xavier Tavares | Lactam kinase inhibitors |
| US20150110723A1 (en) | 2012-05-31 | 2015-04-23 | Emory University | Quinazoline derivatives, compositions, and uses related thereto |
| CN104487429B (en) | 2012-07-27 | 2017-07-14 | 爱默蕾大学 | Heterocycle chromocor derivative, composition and relative method |
| US9676756B2 (en) | 2012-10-08 | 2017-06-13 | Portola Pharmaceuticals, Inc. | Substituted pyrimidinyl kinase inhibitors |
| US9877981B2 (en) | 2012-10-09 | 2018-01-30 | President And Fellows Of Harvard College | NAD biosynthesis and precursors for the treatment and prevention of cancer and proliferation |
| ES2823237T3 (en) | 2012-11-05 | 2021-05-06 | Univ Emory | 7,8-dihydroxyflavone and 7,8-substituted flavone derivatives, compositions and methods related thereto |
| WO2014072419A1 (en) | 2012-11-08 | 2014-05-15 | Universiteit Antwerpen | Novel anti-hiv compounds |
| ES2629762T3 (en) | 2013-01-29 | 2017-08-14 | Redx Pharma Plc | Pyridine derivatives as mild ROCK inhibitors |
| JP2016510797A (en) | 2013-03-15 | 2016-04-11 | オンコデザイン エス.ア. | Macrocyclic salt-inducible kinase inhibitor |
| US9572815B2 (en) | 2013-03-15 | 2017-02-21 | St. Jude Children's Research Hospital | Methods and compositions of p27KIP1 transcriptional modulators |
| EP2967050A4 (en) | 2013-03-15 | 2016-09-28 | G1 Therapeutics Inc | HIGHLY ACTIVE ANINEEOPLASTIC AND ANTIPROLIFERATIVE AGENTS |
| SI2968290T1 (en) | 2013-03-15 | 2020-02-28 | G1 Therapeutics, Inc., | Transient protection of normal cells during chemotherapy |
| KR101548803B1 (en) * | 2013-09-09 | 2015-09-01 | 경북대학교병원 | A pharmaceutical composition for prevention or treatment of diabetes comprising 3-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzamide or pharmaceutically acceptable salts thereof as an effective component |
| SI3043803T1 (en) | 2013-09-11 | 2022-09-30 | Emory University | Nucleotide and nucleoside compositions and their use |
| US10188738B2 (en) | 2013-10-16 | 2019-01-29 | Université Libre de Bruxelles | Formulations useful in the treatment of proliferative diseases affecting the respiratory tract |
| CN103588758A (en) * | 2013-11-04 | 2014-02-19 | 南京大学 | Synthesis and preparation of nitroimidazole derivative containing 1,4-benzdioxan skeleton and application of nitroimidazole derivative in anticancer drugs |
| US10159755B2 (en) | 2013-11-12 | 2018-12-25 | Vrije Universiteit Brussel | RNA transcription vector and uses thereof |
| AU2014354643B2 (en) | 2013-11-27 | 2020-03-05 | Redwood Bioscience, Inc. | Hydrazinyl-pyrrolo compounds and methods for producing a conjugate |
| KR101602203B1 (en) * | 2014-03-11 | 2016-03-11 | 경북대학교병원 | A pharmaceutical composition for prevention or treatment of diabetes comprising n-(2-hydroxyethyl)-3-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzamide or pharmaceutically acceptable salts thereof as an effective component |
| WO2015150472A2 (en) | 2014-04-01 | 2015-10-08 | Université Libre de Bruxelles | New strategies for treating melanoma |
| WO2015150337A1 (en) | 2014-04-01 | 2015-10-08 | Amakem Nv | Lim kinase inhibitors |
| US9717735B2 (en) | 2014-04-17 | 2017-08-01 | G1 Therapeutics, Inc. | Tricyclic lactams for use in HSPC-sparing treatments for RB-positive abnormal cellular proliferation |
| US9980936B2 (en) | 2014-05-05 | 2018-05-29 | Emory University | BH4 antagonists and methods related thereto |
| EP3143005B1 (en) | 2014-05-16 | 2021-07-07 | Emory University | Chemokine cxcr4 and ccr5 receptor modulators and used related thereto |
| EP3180003B1 (en) | 2014-07-01 | 2022-01-12 | The Regents of the University of California | Pkc-epsilon inhibitors |
| US10023602B2 (en) | 2014-07-08 | 2018-07-17 | Universiteit Gent | Hamamelitannin analogues and uses thereof |
| WO2016040848A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors |
| WO2016040858A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| BR112017005299A2 (en) | 2014-09-17 | 2017-12-12 | Ipsen Pharma Sas | macrocyclic lrrk2 kinase inhibitors |
| MY186523A (en) | 2014-09-17 | 2021-07-24 | Oncodesign Sa | Macrocyclic rip2 kinase inhibitors |
| WO2016083490A1 (en) | 2014-11-27 | 2016-06-02 | Remynd Nv | Compounds for the treatment of amyloid-associated diseases |
| SG10202013032YA (en) | 2014-12-15 | 2021-02-25 | Univ Emory | Phosphoramidates for the treatment of hepatitis b virus |
| SG11201705069YA (en) | 2014-12-26 | 2017-07-28 | Univ Emory | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
| WO2016146651A1 (en) | 2015-03-16 | 2016-09-22 | Oncodesign Sa | Macrocyclic activin-like receptor kinase inhibitors |
| ES2927894T3 (en) | 2015-04-28 | 2022-11-11 | Newsouth Innovations Pty Ltd | Targeting of NAD+ to treat cognitive impairment, induced by chemotherapy and radiotherapy, neuropathies and inactivity |
| EP4272820A3 (en) | 2015-05-29 | 2024-01-03 | Emory University | 2-amino-n'-benzylideneacetohydrazides and derivatives for the management of cftr protein mediated diseases |
| JP6902025B2 (en) | 2015-06-18 | 2021-07-14 | ティン セラピューティックス エルエルシー | Methods and compositions for the prevention and treatment of hearing loss |
| JP6855496B2 (en) | 2015-11-09 | 2021-04-07 | アール.ピー.シェーラー テクノロジーズ エルエルシー | Anti-CD22 antibody-Maytan synconjugate and how to use it |
| DK3423113T3 (en) | 2016-02-29 | 2020-11-30 | Oncodesign Sa | RADIO LABEL MACROCYCLIC EGFR INHIBITOR |
| WO2017157882A1 (en) | 2016-03-14 | 2017-09-21 | Université Catholique de Louvain | Serine biosynthetic pathway inhibitors |
| WO2017161253A1 (en) * | 2016-03-18 | 2017-09-21 | Tufts Medical Center | Compositions and methods for treating and preventing metabolic disorders |
| JP7129703B2 (en) | 2016-04-28 | 2022-09-02 | エモリー ユニバーシティー | Alkyne-Containing Nucleotide and Nucleoside Therapeutic Compositions and Uses Associated Therewith |
| US11166967B2 (en) | 2016-05-19 | 2021-11-09 | Universiteit Antwerpen | Bis(acetamidophenyl) guanidinophenylethylphosphonates for use in the prevention and/or treatment of PAR-related diseases |
| BE1023757B1 (en) | 2016-06-30 | 2017-07-12 | Yun NV | STORAGE OF MICRO-ORGANISMS |
| WO2018065387A1 (en) | 2016-10-04 | 2018-04-12 | Universiteit Gent | Novel hamamelitannin analogues and uses thereof |
| EP3532488A4 (en) | 2016-10-14 | 2020-04-29 | Emory University | NANOPARTICLES HAVING MOLECULES THAT BIND OR BLOCK PD-L1 AND THEIR USES IN THE TREATMENT OF CANCER |
| WO2018081442A1 (en) | 2016-10-26 | 2018-05-03 | Emory University | Polyoxometalate complexes and uses in managing cancer |
| EP3544952B1 (en) | 2016-11-24 | 2024-11-06 | Universiteit Antwerpen | Halogenated benzotropolones as atg4b inhibitors |
| WO2018111580A1 (en) | 2016-12-13 | 2018-06-21 | Emory University | Polypeptides for managing viral infections |
| MX2019008158A (en) | 2017-01-06 | 2019-12-09 | G1 Therapeutics Inc | Combination therapy for the treatment of cancer. |
| US20190388426A1 (en) | 2017-01-30 | 2019-12-26 | Université de Liège | Perk and ire-1a inhibitors against neurodevelopmental disorders |
| EP3585387A4 (en) | 2017-02-21 | 2020-08-12 | Emory University | CHEMOKIN CXCR4 RECEPTOR MODULATORS AND USE THEREOF |
| WO2018160967A1 (en) * | 2017-03-02 | 2018-09-07 | Board Of Regents, The University Of Texas System | Indolinone derivatives as inhibitors of maternal embryonic leucine zipper kinase |
| CN106977508A (en) * | 2017-05-05 | 2017-07-25 | 遵义医学院 | Pyrazole derivatives with isatin structure are used for the medicine and its preparation method of anti-curing oncoma |
| EP3634407A1 (en) | 2017-05-11 | 2020-04-15 | Remynd N.V. | Inhibitors of pde6delta for use in the prevention and/or treatment of epilepsy and/or neurodegenerative disorders |
| PL3621963T3 (en) | 2017-05-11 | 2024-05-20 | Remynd N.V. | Compounds for the treatment of epilepsy, neurodegenerative disorders and other cns disorders |
| US11661581B2 (en) * | 2017-05-25 | 2023-05-30 | University Of Massachusetts | Use of CDK inhibitors to enhance growth and self-renewal of progenitor cells |
| CA3067873A1 (en) | 2017-06-29 | 2019-01-03 | G1 Therapeutics, Inc. | Morphic forms of g1t38 and methods of manufacture thereof |
| WO2019113462A1 (en) | 2017-12-07 | 2019-06-13 | Emory University | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
| CA3135420A1 (en) | 2018-04-05 | 2019-10-10 | Universiteit Hasselt | Selective pde4d inhibitors against demyelinating diseases |
| CN112654367B (en) | 2018-06-29 | 2023-08-04 | 再青春生物医药公司 | Drug Combinations for Age-Related and/or Degenerative Diseases |
| EP4344743A3 (en) | 2018-08-07 | 2024-06-19 | Emory University | Heterocyclic flavone derivatives, compositions, and methods related thereto |
| KR20210049847A (en) | 2018-08-24 | 2021-05-06 | 쥐원 쎄라퓨틱스, 인크. | Improved synthesis of 1,4-diazaspiro[5.5]undecan-3-one |
| EP3843845A4 (en) | 2018-08-29 | 2022-05-11 | University Of Massachusetts | INHIBITION OF PROTEIN KINASES TO TREAT FRIEDREICH'S DISEASE |
| WO2020070331A1 (en) * | 2018-10-05 | 2020-04-09 | Ichnos Sciences S.A. | Indolinone compounds for use as map4k1 inhibitors |
| AU2020242053C1 (en) | 2019-03-20 | 2025-11-13 | Emory University | Prostaglandin receptor EP2 antagonists, derivatives, and uses related thereto |
| AU2020274407B2 (en) | 2019-05-14 | 2023-09-28 | Suzhou Four Health Pharmaceuticals Co., Ltd | Quinazoline-2,4-dione derivatives as PARP inhibitors |
| EP3976029A4 (en) | 2019-05-24 | 2023-06-14 | Emory University | ASPARAGIN ENDOPEPTIDASE (AEP) INHIBITORS, COMPOSITIONS AND RELATED USES |
| AU2020315812B2 (en) * | 2019-07-22 | 2025-10-02 | Radius Pharmaceuticals, Inc. | Estrogen receptor-modulating compounds |
| MX2022010413A (en) | 2020-02-24 | 2022-09-07 | Univ Leuven Kath | Pyrrolopyridine and imidazopyridine antiviral compounds. |
| GB202003240D0 (en) | 2020-03-05 | 2020-04-22 | Ecosynth Nv | Antiviral treatment |
| EP4121121A4 (en) | 2020-03-16 | 2024-09-25 | Emory University | RADIONUCLIDES TRACERS OF 1-AMINO-3,4-DIFLUOROCYCLOPENTANE-1-CARBOXYLIC ACID, THEIR DERIVATIVES AND THEIR USES |
| US10988479B1 (en) | 2020-06-15 | 2021-04-27 | G1 Therapeutics, Inc. | Morphic forms of trilaciclib and methods of manufacture thereof |
| WO2022020114A2 (en) | 2020-07-10 | 2022-01-27 | Ting Therapeutics Llc | Methods for the prevention and treatment of hearing loss |
| WO2022157381A1 (en) | 2021-01-25 | 2022-07-28 | Universiteit Hasselt | Phloretin for use in the treatment of neurodegenerative and demyelinating diseases |
| KR20220128285A (en) * | 2021-03-12 | 2022-09-20 | 주식회사 온코크로스 | Composition for the treatment of anticancer drug-resistant cancer |
| CA3227191A1 (en) | 2021-07-26 | 2023-02-02 | Celcuity Inc. | 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea (gedatolisib) and its combinations for use in the treatment of cancer |
| PE20241304A1 (en) | 2021-07-30 | 2024-06-24 | Confo Therapeutics N V | COMPOUNDS FOR THE TREATMENT OF PAIN, PARTICULARLY NEUROPATHIC PAIN, AND/OR OTHER DISEASES OR DISORDERS THAT ARE ASSOCIATED WITH AT2R AND/OR AT2R-MEDIATED SIGNALING |
| EP4387629A1 (en) | 2021-08-18 | 2024-06-26 | Katholieke Universiteit Leuven KU Leuven Research & Development | 6-substituted- and 6,7-disubstituted-7-deazapurine ribonucleoside analogues |
| WO2023046900A1 (en) | 2021-09-23 | 2023-03-30 | Katholieke Universiteit Leuven | Ribonucleoside analogues against -sars-cov-2 |
| WO2023105283A1 (en) | 2021-12-08 | 2023-06-15 | Fundacio Privada Institut De Recerca De La Sida - Caixa | Nucleoside reverse transcriptase inhibitors for use in down syndrome and alzheimer`s disease therapy |
| WO2023111683A1 (en) | 2021-12-16 | 2023-06-22 | Ascletis Bioscience Co., Ltd. | N4-hydroxycytidine derivatives and use thereof as antiviral agent |
| US11541071B1 (en) | 2021-12-16 | 2023-01-03 | Ascletis BioScience Co., Ltd | Nucleoside derivatives and methods of use thereof |
| US11760722B2 (en) | 2022-01-18 | 2023-09-19 | Ascletis Bioscience Co., Ltd. | Inhibitors of cysteine proteases and methods of use thereof |
| WO2023139402A1 (en) | 2022-01-18 | 2023-07-27 | Ascletis Bioscience Co., Ltd. | Inhibitors of cysteine proteases and methods of use thereof |
| WO2023180567A1 (en) | 2022-03-24 | 2023-09-28 | Fundacion Privada Institut De Recerca De La Sida-Caixa | Cyclodextrins for use in coronavirus infection therapy |
| WO2023241799A1 (en) | 2022-06-15 | 2023-12-21 | Université Libre de Bruxelles | Flavanols for use in the treatment of retroviral infections |
| WO2024009120A1 (en) | 2022-07-08 | 2024-01-11 | Ascletis Bioscience Co., Ltd. | Triazine derivatives and methods of use thereof |
| CN117700397A (en) * | 2022-11-02 | 2024-03-15 | 徐诺药业(南京)有限公司 | 2-oxo indoline derivative and preparation method and application thereof |
| CN115504968B (en) | 2022-11-21 | 2023-04-18 | 歌礼生物科技(杭州)有限公司 | Triazine derivatives |
| WO2024193451A1 (en) | 2023-03-17 | 2024-09-26 | Ascletis BioScience Co., Ltd | Triazine derivatives, method of making and method of using thereof |
| WO2025104221A1 (en) | 2023-11-15 | 2025-05-22 | Université Libre de Bruxelles | Uses of protein tyrosine phosphatase receptor kappa inhibitors |
| WO2025155711A1 (en) * | 2024-01-17 | 2025-07-24 | The Board Of Trustees Of The Leland Stanford Junior University | Lrrk2 inhibitors and compositions and uses thereof |
| WO2026013165A1 (en) | 2024-07-10 | 2026-01-15 | Université Libre de Bruxelles | Combination of ship2 inhibitor and plk1 inhibitor for use in the treatment of cancer |
Family Cites Families (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2447940A1 (en) | 1979-02-05 | 1980-08-29 | Ato Chimie | NOVEL FIRE RESISTANT (CO) POLYCARBONATES CONTAINING ALKALINE DIESTER OR HEMIESTER FUNCTIONS OF PHOSPHONIC ACIDS |
| US4971996A (en) * | 1987-03-11 | 1990-11-20 | Kanegafuchi Kagaku Kogyo Kabushiki Kaisha | Hydroxystyrene compounds which are useful as tyrosine kinase inhibitors |
| US5089516A (en) | 1987-03-11 | 1992-02-18 | Kanegafuchi Kagaku Kogyo Kabushiki Kaisha | 1-phenyl-3,5-pyrazolidinedione hydroxystyrene compounds which have tyrosine kinase inhibiting activity |
| US5202341A (en) | 1987-03-11 | 1993-04-13 | Kanegafuchi Kagaku Kogyo Kabushiki Kaisha | Hydroxystyrene compounds having tyrosine kinase inhibiting activity |
| GB8816944D0 (en) * | 1988-07-15 | 1988-08-17 | Sobio Lab | Compounds |
| IE900394L (en) | 1989-02-08 | 1990-08-08 | Abbott Lab | Thiazole derivatives |
| WO1991009598A1 (en) | 1990-01-05 | 1991-07-11 | Pfizer Inc. | Azaoxindole derivatives |
| GB9004483D0 (en) | 1990-02-28 | 1990-04-25 | Erba Carlo Spa | New aryl-and heteroarylethenylene derivatives and process for their preparation |
| US5164404A (en) | 1991-03-15 | 1992-11-17 | Neurosearch A/S | Hydrazone derivatives and their use |
| EP0584264A1 (en) | 1991-05-16 | 1994-03-02 | Cold Spring Harbor Laboratory | D-type cyclin and uses related thereto |
| GB9115160D0 (en) | 1991-07-12 | 1991-08-28 | Erba Carlo Spa | Methylen-oxindole derivatives and process for their preparation |
| US5449755A (en) | 1991-09-20 | 1995-09-12 | Fred Hutchinson Cancer Research Center | Human cyclin E |
| US5441880A (en) | 1991-11-18 | 1995-08-15 | Cold Spring Harbor Laboratory | Human cdc25 genes, encoded products and uses thereof |
| US5770423A (en) | 1991-11-18 | 1998-06-23 | Cold Spring Harbor Laboratory | Nucleic acids encoding cdc25 A and cdc25 B proteins and method of making cdc25 A and cdc25 B proteins |
| US5294538A (en) | 1991-11-18 | 1994-03-15 | Cold Spring Harbor Labs. | Method of screening for antimitotic compounds using the CDC25 tyrosine phosphatase |
| WO1993024514A1 (en) | 1992-05-26 | 1993-12-09 | Mitotix | D-type cyclin and uses related thereto |
| WO1994023029A1 (en) | 1993-03-31 | 1994-10-13 | Monash University | A nucleotide sequence encoding a chromosomal protein, associated chromosomal proteins and their uses |
| US5443962A (en) | 1993-06-04 | 1995-08-22 | Mitotix, Inc. | Methods of identifying inhibitors of cdc25 phosphatase |
| GB9313638D0 (en) | 1993-07-01 | 1993-08-18 | Erba Carlo Spa | Arylidene and heteroarylidene oxindole derivatives and process for their preparation |
| GB9412719D0 (en) | 1994-06-24 | 1994-08-17 | Erba Carlo Spa | Substituted azaindolylidene compounds and process for their preparation |
| US5496828A (en) * | 1994-08-22 | 1996-03-05 | Eli Lilly And Company | Methods of inhibiting ulcerative mucositis |
| CA2235810C (en) | 1994-10-24 | 2010-02-09 | Baylor College Of Medicine | Senescent cell-derived inhibitors of dna synthesis |
| GB9423997D0 (en) | 1994-11-28 | 1995-01-11 | Erba Carlo Spa | Substituted 3-arylidene-7-azaoxindole compounds and process for their preparation |
| GB9501567D0 (en) | 1995-01-26 | 1995-03-15 | Pharmacia Spa | Hydrosoluble 3-arylidene-2-oxindole derivatives as tyrosine kinase inhibitors |
| GB9507298D0 (en) | 1995-04-07 | 1995-05-31 | Pharmacia Spa | Substituted indolylmethylene-oxindale analogues as tyrosine kinase inhibitors |
| US5880141A (en) | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
| EP0815859B1 (en) | 1996-01-17 | 2003-06-18 | Taiho Pharmaceutical Company Limited | Intimal thickening inhibitors |
| US5672508A (en) | 1996-01-23 | 1997-09-30 | Mitotix, Inc. | Inhibitors of cell-cycle progression, and uses related thereto |
| EP0788890A1 (en) | 1996-02-06 | 1997-08-13 | Agfa-Gevaert N.V. | Dyes and dye-donor elements for thermal dye transfer recording |
| CN1128788C (en) | 1996-03-29 | 2003-11-26 | 辉瑞大药厂 | Benzyl(idene)-lactam derivatives, their prepn. and their use as selective (ant) agaonists of 5-ht1A-and/or 5-ht1D receptors |
| WO1998007835A2 (en) | 1996-08-21 | 1998-02-26 | Sugen, Inc. | Crystal structures of a protein tyrosine kinase |
| CA2264220A1 (en) | 1996-08-23 | 1998-02-26 | Sugen, Inc. | Indolinone combinatorial libraries and related products and methods for the treatment of disease |
| WO1998050356A1 (en) * | 1997-05-07 | 1998-11-12 | Sugen, Inc. | 2-indolinone derivatives as modulators of protein kinase activity |
| GB9718913D0 (en) * | 1997-09-05 | 1997-11-12 | Glaxo Group Ltd | Substituted oxindole derivatives |
| US6319918B1 (en) * | 1998-06-04 | 2001-11-20 | Boehringer Ingelheim Pharma Kg | Substituted indolinones with kinase inhibitory activity |
| GB9904932D0 (en) * | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Composition and method for preventing/reducing the severity of side effects of chemotherapy and/or radiation therapy |
| GB9904930D0 (en) * | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Thiazoloindolinone compounds |
| GB9904933D0 (en) * | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Compounds |
| US6620818B1 (en) * | 2000-03-01 | 2003-09-16 | Smithkline Beecham Corporation | Method for reducing the severity of side effects of chemotherapy and/or radiation therapy |
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1997
- 1997-09-05 GB GBGB9718913.8A patent/GB9718913D0/en active Pending
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1998
- 1998-08-25 TW TW087113993A patent/TW520358B/en active
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| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
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